ChemicalBook--->CAS DataBase List--->1035638-91-5

1035638-91-5

1035638-91-5 Structure

1035638-91-5 Structure
IdentificationBack Directory
[Name]

PF-6274484
[CAS]

1035638-91-5
[Synonyms]

PF-6274484
PF-6274484 >=98% (HPLC)
N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-2-propenamide
2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-
[Molecular Formula]

C18H14ClFN4O2
[MDL Number]

MFCD30182370
[MOL File]

1035638-91-5.mol
[Molecular Weight]

372.78
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 33 mg/ml; DMSO: 25 mg/ml
[form ]

A crystalline solid
[color ]

Light yellow to orange
Hazard InformationBack Directory
[Description]

PF-6274484 is an irreversible EGFR kinase inhibitor that covalently reacts with active-site cysteine residues in the ATP binding pocket. PF-6274484 inhibits autophosphorylation of both wild type and mutant EGFR in tumor cells with IC50 values of 5.8 nM and 6.6 nM, respectively.
[Uses]

PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively[1].
[IC 50]

EGFR (WT): 0.18 nM (Ki); EGFRL858R/T790M: 0.14 nM (Ki)
[storage]

Store at -20°C
[References]

[1] Schwartz PA, et al. Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc Natl Acad Sci U S A. 2014;111(1):173-178. DOI:10.1073/pnas.1313733111
Spectrum DetailBack Directory
[Spectrum Detail]

PF-6274484(1035638-91-5)1HNMR
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